ABSTRACT
This research aims to explore the saponins composition of H. nepalensis in four northwest mountainous areas of Vietnam including Ha Giang, Lai Chau, Lao Cai, and Lang Son with the aid of high-resolution mass spectrometry. As a result, 42 saponins are successfully identified in H. nepalensis leaves by UHPLC-Q-TOF-MS/MS analyses, in which two 30-noroleanane and four oleanane triterpene saponins structures have been reported for the first time. Two structures of compound 20 were discovered in four samples. Two structures of compound 8 were found in H. nepalensis from Ha Giang and Lao Cai, while two structures of compound 28 were not observed in Lang Son. Different environmental and climatic circumstances in various places may have an impact on chemical constituents of H. nepalensis. By providing the phytochemicals profile of H. nepalensis leaves, our study supports the orientation for future research on this medicinal plant as well as other Hedera species.
ABSTRACT
In this study, we found that the hexane fraction of Danshen, the dried root of Salvia miltiorrhiza (Lamiaceae), exerted antiproliferative effects on human leukemia cells. Phytochemical investigation of the hexane fraction achieved the isolation of the tanshinone diterpenes: dihydrotanshinone I (1), trijuganone C (2), trijuganone B (3), cryptotanshinone (4), tanshinone IIA (5), and tanshinone I (6). Compound 2 showed significant antiproliferative activities against human leukemia cells HL-60, Jurkat, and U937. The antiproliferative activities of 2 against human cancer and normal cells indicated that 2 exhibited potent antiproliferative activities with IC50 values less than 10 µM against HL-60 and Jurkat cells as well as on the colon cancer cells DLD-1, COLO 205, and Caco-2. Compound 2 induced chromatin condensation, DNA fragmentation, activation of caspase-3, -8, and -9, and the cleavage of poly (ADP-ribose) polymerase (PARP) in HL-60 cells. Moreover, 2 activated Bid and Bax, leading to the loss of mitochondrial membrane potential, and 2 induced the cytochrome c release from mitochondria into cytosol. In contrast, Bcl-2 and Bcl-xL were unaffected by 2. These results suggest that 2 exerts antiproliferative effects via apoptosis induction mediated by mitochondrial dysfunction and caspase activation. Compound 2 may serve as a candidate of potential chemotherapeutic agent for human leukemia.
Subject(s)
Phenanthrenes/chemistry , Plant Roots/chemistry , Salvia miltiorrhiza/chemistry , Apoptosis , HumansABSTRACT
Danshen (Salvia miltiorrhiza) is a well-known medicinal herb in the oriental medicine. The current study on bioactive triterpenoid in the root of S. miltiorrhiza led to the isolation of a new highly hydroxylated ursane-type triterpene, urs-12-ene-2α,3ß,7ß,16α-tetraol (1) and five known ones including 2ß-hydroxypomolic acid (2), maslinic acid (3), asiatic acid (4), ursolic acid (5), and oleanolic acid (6). Their structures were elucidated on the basis of extensive spectroscopic analyses and comparison with literature data. The antiproliferative testing against HL-60 cells revealed that the new compound 1 and ursolic acid (5) showed weak and moderate activities with IC50 values of 42.2 and 11.7 µM. In addition, compounds 1-3 showed inhibitory effect on ghrelin activity. Copyright © 2017 John Wiley & Sons, Ltd.
